帕布昔利布和氟维司群共载药阳离子脂质体的制备和性质评价

Preparation and Characterization of Cationic Liposomes Co-loaded with Palbociclib and Fulvestrant

制备帕布昔利布(Pal)和氟维司群(Ful)共载药阳离子脂质体(cationic liposomes,CLs),对其物理化学性质进行表征.以二油酰磷脂酰乙醇胺和(2,3-二油酰基-丙基)-三甲胺为膜材,采用薄膜分散法制备帕布昔利布和氟维司群共载药阳离子脂质体(CLs),HPLC法测定共载药阳离子脂质体的包封率和载药量,激光粒度仪考察脂质体粒径和电位的分布情况,透射电子显微镜观察脂质体的形态.结果表明:Pal-Ful-CLs的平均粒径为(182.13±3.56)nm,多分散系数为0.18±0.02,表明分散度良好;Pal-Ful-CLs的电位为(57.1±2.6)mV,阳离子脂质体表面的正电荷有利于脂质体在体系中的均匀分散和稳定;在透射电子显微镜下观察到脂质体呈圆形且粒径与粒度仪测定结果一致.本研究制备的共载药阳离子脂质体粒径均一、分散稳定并且工艺重现性好,作为药物共同递送载体具有一定的应用前景.

A novel type of cationic liposomes(CLs)co-loaded with pabuccilib(Pal)and fulvestrant(Ful)were prepared and their physicochemical properties were characterized in this study.With the dioleoyl phosphatidylethanolamine and(2,3-dioleoyl-propyl)-trimethylamine as membrane materials,a thin film dispersion method was used to prepare the cationic lipo-somes(CLs)co-drug-loaded cationic lipids of Pal and Ful HPLC method was used to determine the entrapment efficiency and drug loading of co-drug-loaded cationic liposomes;laser particle size analyzer was used to investigate the particle sizeand potential distribution of liposomes;the morphology of liposomes was observed by transmission electron microscope.Theresult of the study showed that the average particle size of Pal-Ful-CLs was(182.13±3.56)nm,and the polydispersity coeffi-cient was 0.18±0.02,indicating good dispersion;the potential of Pal-Ful-CLs was(57.1±2.6)mV,cationic liposomes The positive charge on the surface is beneficial to the uniform and stable dispersion of liposomes in the system;under the TEM,it was observed that the liposomes were round and the particle size was consistent with the results of the particle size analyzer.The co-drug-loaded cationic liposomes prepared in this study have uniform particle size,stable dispersion and good process reproducibility.They have certain application prospects as a drug delivery vehicle.